Regimen is considered appropriate as part of the standard care of patients; meaningfully improves outcomes (survival, quality of life), tolerability or costs compared to alternatives (recommended by the Disease Site Team and national consensus body e.g. pan-Canadian Oncology Drug Review, pCODR). Recommendation is based on an appropriately conducted phase III clinical trial relevant to the Canadian context OR (where phase III trials are not feasible) an appropriately sized phase II trial. Regimens where one or more drugs are not approved by Health Canada for any indication will be identified under Rationale and Use.
- For the treatment of metastatic, castrate-resistant prostate cancer (mCRPC) in combiation with ADT and prednisone, in patients who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy, have no history of viral hepatitis / chronic liver disease / significant cardiac disease and have not received prior chemotherapy (EAP criteria)
- For the treatment of metastatic, castrate-resistant prostate cancer in combination with ADT and prednisone, in patients who have progressed after prior chemotherapy containing docetaxel
- Abiraterone is not funded for combination treatment with cabazitaxel or enzalutamide, in patients who have received prior chemotherapy for mCRPC or in newly diagnosed hormone-sensitive high-risk metastatic prostate cancer
|abiraterone||1000 mg||PO||once daily|
(Outpatient prescription in 250 mg and 500 mg tablets)
|10 mg||PO||once daily|
(Outpatient prescription in 5 mg tablets)
Patients should continue to receive GnRH agonists during abiraterone treatment unless they have had prior orchiectomy.
Other Supportive Care:
- May require increased corticosteroid dosage before, during and after periods of unusual stress such as surgery or trauma
Doses should be modified according to the protocol by which the patient is being treated. Control hypertension and correct hypokalemia before treatment.
Dosage with toxicity
Grade 3 ALT/AST
Grade 3 total bilirubin
Hold; monitor liver function closely until recovery to baseline THEN
Reduce to 500mg/day
Grade 4 ↑ LFTs
ALT/AST > 3 x ULN AND total bilirubin > 2 x ULN (in the absence of biliary obstruction or other causes)
OR ≥ Grade 3 ↑ LFTs after dose modification
OR confirmed pneumonitis/allergic alveolitis
|Discontinue permanently||Not applicable||Not applicable|
|Toxicity (continued)||Action||Abiraterone dose||Prednisone dose|
|Hypokalemia persists despite optimal K supplements and adequate oral intake
Other mineralcorticoid effects persist
|No change||If on 5mg/day, may increase to 10 mg/day|
Increased exposure and half-life have been observed in patients with hepatic impairment at baseline; abiraterone has not been studied in patients with moderate or severe hepatic impairment and should not be used. (Patients with moderate to severe hepatic impairment, active hepatitis, chronic liver disease or ascites were excluded from clinial trials.)
Refer to the table above for dose modifications with hepatotoxicity during treatment.
No dose adjustment required for prednisone.
|Hepatic Impairment (at baseline)||Dose|
|Mild (Child-Pugh Class A)||No change|
|Moderate (Child-Pugh Class B)||Do not use abiraterone|
|Severe (Child-Pugh Class C)||Do not use abiraterone|
No dose adjustment required for prednisone or abiraterone.
Dosage in the Elderly
No overall differences in effectiveness or adverse effects were seen between elderly and younger patients.
Very common (≥ 50%)
Less common (10-24%)
Uncommon (< 10%),
but may be severe or life-threatening
Refer to abiraterone drug monograph(s) for additional details
- Avoid co-administration with CYP2D6 substrates with narrow therapeutic range due to increased risk of toxicity. If must co-administer, consider dose reduction of 2D6 substrate.
- Avoid strong CYP3A4 inducers due to risk of reduced efficacy.
- Avoid strong CYP3A4 inhibitors due to increased risk of toxicity.
- Avoid spironolactone as this may stimulate disease progression.
- Caution when co-administered with drugs that increase risk of myopathy/rhabdomyolysis
Refer to abiraterone, prednisone drug monograph(s) for additional details
- Abiraterone must be taken on an empty stomach. No solid or liquid food should be eaten for at least 2 hours before and at least 1 hour after the dose.
- The tablets should be swallowed whole with a glass of water.
- If an abiraterone dose is missed, skip this and take the next dose as scheduled. Do not double the dose to make up for the missed one.
- Since abiraterone may harm the fetus, women who are pregnant or who may become pregnant should handle abiraterone with protection (e.g. gloves).
- Women who are or may potentially be pregnant (not for use in women)
- Patients who have a hypersensitivity to this drug or any of its components
- Moderate-severe hepatic impairment at baseline
- Severe (grade 4) hepatotoxicity
- Use with caution in patients with cardiovascular disease as they were not included in clinical trials. Increased mineralocorticoid levels from CYP17 inhibition may cause hypertension, hypokalemia and fluid retention. Use with caution in patients whose underlying medical conditions may be affected by these effects.
- Use with caution in patients taking other medications associated with myopathy or rhabdomyolysis (e.g. statins)
- Adrenal insufficiency has been reported in patients taking abiraterone and prednisone. Increased corticosteroid dosage may be required before, during and after the stressful situation.
- Contains lactose and should not be used in patients with hereditary galactose intolerance, severe lactase deficiency or glucose-galactose malabsorption.
- Efficacy may be lower in patients who have been treated previously with ketoconazole for their prostate cancer.
- The safety and efficacy of combination abiraterone and cytotoxic chemotherapy use has not been established.
Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.
Recommended Clinical Monitoring
- Blood pressure, serum potassium; baseline and monthly
- Cholesterol and triglycerides; baseline, every 2 to 3 months and as clinically indicated.
- Liver function tests, bilirubin; baseline, every 2 weeks for the first 3 months and monthly thereafter, or as clinically indicated
- Monitor for adrenal insufficiency; as clinically indicated when prednisone is withdrawn, or during periods of infection/stress
- Monitor for mineralocorticoid excess; as clinically indicated if patient continues on abiraterone after stopping prednisone
- Clinical toxicity assessment for hypertension, edema, GI, musculoskeletal or steroid side effects, hot flashes, urinary symptoms, cardiac and respiratory toxicity; at each visit
Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version
Abiraterone drug monograph, Cancer Care Ontario.
de Bono JS., Logothetis CJ, Molina A, et al. Abiraterone and increased survival in metastatic prostate cancer. N Engl J Med 2011;364:1995-2005.
Ryan CJ, Smith MR, de Bono JS, et al. Abiraterone in metastatic prostate cancer without previous chemotherapy. N Engl J Med 2013;368(2):138-48.
July 2018 Updated rationale and use, dose modifications, adverse effects, contraindications sections
A Regimen Abstract is an abbreviated version of a Regimen Monograph and contains only top level information on usage, dosing, schedule, cycle length and special notes (if available). It is intended for healthcare providers and is to be used for informational purposes only. It is not intended to constitute or be a substitute for medical advice, and all uses of the Regimen Abstract are subject to clinical judgment. Such information is provided on an “as-is” basis, without any representation, warranty, or condition, whether express, or implied, statutory or otherwise, as to the information’s quality, accuracy, currency, completeness, or reliability, and Cancer Care Ontario disclaims all liability for the use of this information, and for any claims, actions, demands or suits that arise from such use.
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